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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: hypotension, QTc interval prolongation

GI: nausea, dysphagia

Neuro: akathisia, balance difficulty, dysarthria, parkinsonism, unsteady gait, anxiety, fatigue, insomnia, depression, sedation/somnolence, cognitive defects, dizziness, headache

Resp: dyspnea

Misc: NEUROLEPTIC MALIGNANT SYNDROME

Interactions

Drug-drug:

Availability

(Generic available)

Route/Dosage

US Brand Names

Xenazine

Action

  • Acts as a reversible inhibitor of the vesicle monoamine transporter type 2 (VMAT-2); which inhibits the reuptake of serotonin, norepinephrine and dopamine into vesicles in presynaptic neurons.
Therapeutic effects:
  • Decreased chorea due to Huntington's Disease.

Classifications

Therapeutic Classification: antichoreas

Pharmacologic Classification: reversible monoamine depleters

Pharmacokinetics

Absorption: 75% absorbed following oral administration.

Distribution: Crosses the blood-brain barrier.

Metabolism/Excretion: Rapidly and extensively metabolized by the liver; CYP2D6 plays a large role in the metabolic process (the CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers and may have significantly concentrations and an risk of adverse effects). Metabolites are renally excreted. Two metabolites α-dihydrotetrabenazine (α-HTBZ) and β-HTBZ bind to VMAT-2 and are pharmacologically active.

Half-Life: α-HTBZ—4–8 hrs; β-HTBZ—2–4 hr.

Canadian Brand Names

Nitoman

Time/Action Profile

(blood levels)

ROUTEONSETPEAKDURATION
POunknown1.0–1.5 hr12–18 hr*

*Return of symptoms following discontinuation.

Patient/Family Teaching

Pronunciation

te-tra-BEN-a-zeen

Code

NDC Code